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Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
Tseng SL, Hung MS, Chang CP, Song JS, Tai CL, Chiu HH, Hsieh WP, Lin Y, Chung WL, Kuo CW, Wu CH, Chu CM, Tung YS, Chao YS, Shia KS. Tseng SL, et al. Among authors: kuo cw. J Med Chem. 2008 Sep 11;51(17):5397-412. doi: 10.1021/jm800066v. Epub 2008 Aug 20. J Med Chem. 2008. PMID: 18712856
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice.
Wu CH, Hung MS, Song JS, Yeh TK, Chou MC, Chu CM, Jan JJ, Hsieh MT, Tseng SL, Chang CP, Hsieh WP, Lin Y, Yeh YN, Chung WL, Kuo CW, Lin CY, Shy HS, Chao YS, Shia KS. Wu CH, et al. Among authors: kuo cw. J Med Chem. 2009 Jul 23;52(14):4496-510. doi: 10.1021/jm900471u. J Med Chem. 2009. PMID: 19530697
Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.
Yang S, Chen SJ, Hsu MF, Wu JD, Tseng CT, Liu YF, Chen HC, Kuo CW, Wu CS, Chang LW, Chen WC, Liao SY, Chang TY, Hung HH, Shr HL, Liu CY, Huang YA, Chang LY, Hsu JC, Peters CJ, Wang AH, Hsu MC. Yang S, et al. Among authors: kuo cw. J Med Chem. 2006 Aug 10;49(16):4971-80. doi: 10.1021/jm0603926. J Med Chem. 2006. PMID: 16884309
317 results